Debio-1347 - CAS 1265229-25-1
Catalog number: 1265229-25-1
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
FGFR
Description:
Debio-1347, also known as FF284 and CH5183284, is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity. FGFR inhibitor debio 1347 binds to and inhibits FGFR-1, -2, and -3, which result in the inhibition of FGFR-mediated signal transduction pathways. This leads to the inhibition of both tumor cell proliferation and angiogenesis, and causes cell death in FGFR-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases upregulated in many tumor cell types, is essential for tumor cellular proliferation, differentiation and survival.
Publictions citing BOC Sciences Products
  • >> More
Appearance:
Solid powder
Synonyms:
Debio-1347; Debio 1347; Debio1347; CH5183284; CH 5183284; CH-5183284; FF-284; FF284; FF 284.
MSDS:
Inquire
1.ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor.
Nakanishi Y1, Mizuno H2, Sase H2, Fujii T2, Sakata K2, Akiyama N2, Aoki Y2, Aoki M2, Ishii N2. Mol Cancer Ther. 2015 Dec;14(12):2831-9. doi: 10.1158/1535-7163.MCT-15-0497. Epub 2015 Oct 5.
Drugs that target specific gene alterations have proven beneficial in the treatment of cancer. Because cancer cells have multiple resistance mechanisms, it is important to understand the downstream pathways of the target genes and monitor the pharmacodynamic markers associated with therapeutic efficacy. We performed a transcriptome analysis to characterize the response of various cancer cell lines to a selective fibroblast growth factor receptor (FGFR) inhibitor (CH5183284/Debio 1347), a mitogen-activated protein kinase kinase (MEK) inhibitor, or a phosphoinositide 3-kinase (PI3K) inhibitor. FGFR and MEK inhibition produced similar expression patterns, and the extracellular signal-regulated kinase (ERK) gene signature was altered in several FGFR inhibitor-sensitive cell lines. Consistent with these findings, CH5183284/Debio 1347 suppressed phospho-ERK in every tested FGFR inhibitor-sensitive cell line. Because the mitogen-activated protein kinase (MAPK) pathway functions downstream of FGFR, we searched for a pharmacodynamic marker of FGFR inhibitor efficacy in a collection of cell lines with the ERK signature and identified dual-specificity phosphatase 6 (DUSP6) as a candidate marker.
2.The fibroblast growth factor receptor genetic status as a potential predictor of the sensitivity to CH5183284/Debio 1347, a novel selective FGFR inhibitor.
Nakanishi Y1, Akiyama N2, Tsukaguchi T2, Fujii T2, Sakata K2, Sase H2, Isobe T3, Morikami K3, Shindoh H2, Mio T4, Ebiike H2, Taka N3, Aoki Y2, Ishii N2. Mol Cancer Ther. 2014 Nov;13(11):2547-58. doi: 10.1158/1535-7163.MCT-14-0248. Epub 2014 Aug 28.
The FGF receptors (FGFR) are tyrosine kinases that are constitutively activated in a subset of tumors by genetic alterations such as gene amplifications, point mutations, or chromosomal translocations/rearrangements. Recently, small-molecule inhibitors that can inhibit the FGFR family as well as the VEGF receptor (VEGFR) or platelet-derived growth factor receptor (PDGFR) family displayed clinical benefits in cohorts of patients with FGFR genetic alterations. However, to achieve more potent and prolonged activity in such populations, a selective FGFR inhibitor is still needed. Here, we report the identification of CH5183284/Debio 1347, a selective and orally available FGFR1, FGFR2, and FGFR3 inhibitor that has a unique chemical scaffold. By interacting with unique residues in the ATP-binding site of FGFR1, FGFR2, or FGFR3, CH5183284/Debio 1347 selectively inhibits FGFR1, FGFR2, and FGFR3 but does not inhibit kinase insert domain receptor (KDR) or other kinases.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related FGFR Products


CAS 939805-30-8 ACTB-1003

ACTB-1003
(CAS: 939805-30-8)

ACTB-1003 is an oral kinase inhibitor with multiple modes of action, targeting cancer mutations via FGFR inhibition FGFR1, angiogenesis through inhibition of VE...

CAS 872511-34-7 BGJ-398

BGJ-398
(CAS: 872511-34-7)

BGJ398, also known as NVP-BGJ398, is a pan FGFR kinase inhibitor, and is an orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs...

CAS 656247-18-6 BIBF 1120 esylate

BIBF 1120 esylate
(CAS: 656247-18-6)

Nintedanib esylate is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β.

CAS 1708971-55-4 FGF-401

FGF-401
(CAS: 1708971-55-4)

FGF-401 is an inhibitor of human fibroblast growth factor receptor 4 (FGFR4) (IC50= 1.9 nM) developed for the treatment of solid tumor.

CAS 1035270-39-3 AZD-4547

AZD-4547
(CAS: 1035270-39-3)

AZD4547 is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. AZD4547 binds to and inhibit...

S-49076
(CAS: 1265965-22-7)

This active molecular is a Axl receptor tyrosine kinase inhibitor, Proto oncogene protein c met inhibitor, Type-1, Type-2 and Type-3 fibroblast growth factor re...

CAS 326914-10-7 SU11652

SU11652
(CAS: 326914-10-7)

SU11652 is a cell-permeable and sunitinib-like inhibitor of tyrosine kinase receptor (RTK) and angiogenesis with antineoplastic property. It selectively inhibit...

CAS 1707289-21-1 BLU-554

BLU-554
(CAS: 1707289-21-1)

BLU-554 is a potent and selective inhibitor of fibroblast growth factor receptor 4 (FGFR4) (IC50 = 5 nM), which is promisingly to be used for the treatment of h...

CAS 192705-80-9 PD-161570

PD-161570
(CAS: 192705-80-9)

PD-161570 is a selective inhibitor of human FGF-1 receptor tyrosine kinase, with IC50 values to be 40, 262 and 3700 nM for FGFR1, PDGFR and EGFR tyrosine kinase...

CAS 9050-30-0 Heparan Sulfate

Heparan Sulfate
(CAS: 9050-30-0)

Heparan sulfate, a complex and linear polysaccharide in which the backbone is composed of repeating sulfated disaccharide units, exists as part of glycoproteins...

CAS 1125780-41-7 SKLB610

SKLB610
(CAS: 1125780-41-7)

SKLB610 is a VEGFR inhibitor that potently suppresses human tumor angiogenesis. SKLB610 inhibited angiogenesis-related tyrosine kinase VEGFR2, fibroblast growth...

FIIN-2
(CAS: 1633044-56-0)

FIIN-2 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. FIIN-2 is the first inhibitor that can potently inhibit the prolife...

ARQ-087
(CAS: 1234356-69-4)

ARQ-087, also known as Derazantinib, is an oral fibroblast growth factor receptor (FGFR) inhibitor with antitumor property. FGFR plays a role in the regulation ...

CAS 1310746-10-1 NVP-BGJ398 phosphate

NVP-BGJ398 phosphate
(CAS: 1310746-10-1)

Potent and selective inhibitor of fibroblast growth factor receptor (FGFR) tyrosine kinases 1, 2, 3 and 4 (with IC50 values of 0.9, 1.4, 1.0 and 60 nM for FGFR1...

CAS 1058137-23-7 Lucitanib

Lucitanib
(CAS: 1058137-23-7)

Lucitanib, also known as E-3810, is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor re...

CAS 1708971-72-5 FGFR4-IN-1

FGFR4-IN-1
(CAS: 1708971-72-5)

FGFR4-IN-1 is a potent and selective FGFR4 inhibitor with potential for the treatment of gastric cancer.

CAS 848463-13-8 SSR128129E free acid

SSR128129E free acid
(CAS: 848463-13-8)

SSR128129E free acid is a multi-FGFR blocker with allosteric properties. It inhibits FGFR signaling by binding to the extracellular FGFR domain without affectin...

BLU9931
(CAS: 1538604-68-0)

BLU9931 is a potent and irreversible small-molecule inhibitor of FGFR4, as a targeted therapy to treat patients with HCC whose tumors have an activated FGFR4 si...

Erdafitinib
(CAS: 1346242-81-6)

Erdafitinib, also known as JNJ-42756493, is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential an...

CAS 692737-80-7 Dovitinib lactate

Dovitinib lactate
(CAS: 692737-80-7)

Dovitinib, also referred as CHIR-258 or TKI258, is a potent receptor tyrosine kinase inhibitor (TKI) that selectively targets VEGFR, PDGFR, FGFR, CSF1R, c-KIT, ...

Chemical Structure

CAS 1265229-25-1 Debio-1347

Quick Inquiry

Verification code

Featured Items